Use of novel boronic acid transition state inhibitors to probe substrate affinity in SHV-type extended-spectrum beta-lactamases.

Abstract:

:Boronic acid transition state inhibitors (BATSIs) with R1 side chains of cefotaxime and ceftazidime were assayed against SHV-1, SHV-2, SHV-5, D104K, and D104K G238S beta-lactamases. The D104K variant was the most susceptible to inhibition by the ceftazidime BATSI (Ki, 730+/-80 nM), while the D104K G238S variant was the most susceptible to the cefotaxime BATSI (Ki, 1.1+/-0.2 microM).

authors

Thomson JM,Prati F,Bethel CR,Bonomo RA

doi

10.1128/AAC.01293-06

subject

Has Abstract

pub_date

2007-04-01 00:00:00

pages

1577-9

issue

4

eissn

0066-4804

issn

1098-6596

pii

AAC.01293-06

journal_volume

51

pub_type

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